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Assay Detail

CHEMBL958182

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL ↗
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL3759) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.
Smits RA, de Esch IJ, Zuiderveld OP, Broeker J, Sansuk K, Guaita E, Coruzzi G, Adami M, Haaksma E, Leurs R.
J Med Chem (2008) 51 : 7855 -7865
PubMed 19053770 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 61 6.67 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373579 — — 1 9.00
CHEMBL129198 JNJ-7777120 — 1 8.38
CHEMBL260549 — — 1 8.25
CHEMBL452847 — — 1 8.12
CHEMBL454890 — — 1 7.57
CHEMBL213912 — — 1 7.55
CHEMBL509852 — — 1 7.47
CHEMBL509142 — — 1 7.45
CHEMBL452869 — — 1 7.41
CHEMBL261551 — — 1 7.40
CHEMBL452848 — — 1 7.22
CHEMBL489062 — — 1 7.15
CHEMBL452925 — — 1 7.05
CHEMBL473302 — — 1 6.98
CHEMBL453877 — — 1 6.98
CHEMBL489070 — — 1 6.98
CHEMBL454891 — — 1 6.97
CHEMBL448962 — — 1 6.89
CHEMBL452849 — — 1 6.87
CHEMBL512568 — — 1 6.85
CHEMBL461537 — — 1 6.81
CHEMBL454883 — — 1 6.73
CHEMBL523941 — — 1 6.73
CHEMBL454882 — — 1 6.65
CHEMBL490072 — — 1 6.62
CHEMBL490071 — — 1 6.59
CHEMBL509961 — — 1 6.57
CHEMBL612059 — — 1 6.57
CHEMBL489464 — — 1 6.44
CHEMBL452870 — — 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373579 — Ki = 1.0 nM 9.00
CHEMBL129198 JNJ-7777120 Ki = 4.169 nM 8.38
CHEMBL260549 — Ki = 5.623 nM 8.25
CHEMBL452847 — Ki = 7.586 nM 8.12
CHEMBL454890 — Ki = 26.92 nM 7.57
CHEMBL213912 — Ki = 28.18 nM 7.55
CHEMBL509852 — Ki = 33.88 nM 7.47
CHEMBL509142 — Ki = 35.48 nM 7.45
CHEMBL452869 — Ki = 38.9 nM 7.41
CHEMBL261551 — Ki = 39.81 nM 7.40
CHEMBL452848 — Ki = 60.26 nM 7.22
CHEMBL489062 — Ki = 70.79 nM 7.15
CHEMBL452925 — Ki = 89.13 nM 7.05
CHEMBL453877 — Ki = 104.71 nM 6.98
CHEMBL473302 — Ki = 104.71 nM 6.98
CHEMBL489070 — Ki = 104.71 nM 6.98
CHEMBL454891 — Ki = 107.15 nM 6.97
CHEMBL448962 — Ki = 128.82 nM 6.89
CHEMBL452849 — Ki = 134.9 nM 6.87
CHEMBL512568 — Ki = 141.25 nM 6.85
CHEMBL461537 — Ki = 154.88 nM 6.81
CHEMBL454883 — Ki = 186.21 nM 6.73
CHEMBL523941 — Ki = 186.21 nM 6.73
CHEMBL454882 — Ki = 223.87 nM 6.65
CHEMBL490072 — Ki = 239.88 nM 6.62
CHEMBL490071 — Ki = 257.04 nM 6.59
CHEMBL612059 — Ki = 269.15 nM 6.57
CHEMBL509961 — Ki = 269.15 nM 6.57
CHEMBL489464 — Ki = 363.08 nM 6.44
CHEMBL452870 — Ki = 371.54 nM 6.43
CHEMBL489271 — Ki = 562.34 nM 6.25
CHEMBL489664 — Ki = 575.44 nM 6.24
CHEMBL489061 — Ki = 588.84 nM 6.23
CHEMBL455133 — Ki = 602.56 nM 6.22
CHEMBL489060 — Ki = 616.6 nM 6.21
CHEMBL488885 — Ki = 691.83 nM 6.16
CHEMBL490073 — Ki = 758.58 nM 6.12
CHEMBL510181 — Ki = 954.99 nM 6.02
CHEMBL489069 — Ki = 954.99 nM 6.02
CHEMBL118572 — Ki = 1071.52 nM 5.97
CHEMBL523617 — Ki = 1479.11 nM 5.83
CHEMBL475331 — Ki = 2137.96 nM 5.67
CHEMBL473098 — Ki = 2818.38 nM 5.55
CHEMBL473099 — Ki = 4073.8 nM 5.39
CHEMBL443764 — Ki = 7585.78 nM 5.12
CHEMBL515870 — Ki = 8511.38 nM 5.07
CHEMBL471712 — Ki = 15135.61 nM 4.82
CHEMBL511699 — Ki > 1000.0 nM -
CHEMBL461732 — Ki > 1000.0 nM -
CHEMBL461360 — Ki > 1000.0 nM -